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首页> 外文学位 >In-vitro assessment of indomethacin release from dermatological formulations using cellulose membrane, excised pig and human cadaver skin barriers.
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In-vitro assessment of indomethacin release from dermatological formulations using cellulose membrane, excised pig and human cadaver skin barriers.

机译：使用纤维素膜，切除的猪和人尸体皮肤屏障从皮肤病学制剂中释放吲哚美辛的体外评估。

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摘要

Indomethacin/Indometacin is a non-steroidal anti-inflammatory drug (NSAID) that exhibits antipyretic and analgesic properties. Indomethacin has been shown to be an effective anti-inflammatory agent, appropriate for long-term use in rheumatoid arthritis, ankylosing spondylitis, and osteoarthritis. Indomethacin is available as a capsule dosage form in three different strengths, 25; 50 and SR 75 mg. It is also available as suspension in the strength of 25 mg/ml and 50 mg suppository.;The main disadvantage of oral non-selective COX inhibitors NSAIDs are they can be toxic to kidney and increases the risk of gastrointestinal bleeding. A population using NSAID's are at increased risk for serious gastrointestinal (GI) complications. NSAIDs such as Indomethacin, Meloxicam, Ibuprofen etc may cause ulcers, bleeding, or holes in the stomach or intestine. The risk of having a heart attack or a stroke is also increased in people who take non-steroidal anti-inflammatory drugs (NSAIDs).;An attempt was made to evaluate the feasibility of developing topical formulations of this drug, as a means to overcome its gastrointestinal complications and cardiovascular risks when administered as an oral dosage form.;Various dermatological formulations of Indomethacin were formulated using bases like HPMC gel and anionic and non-ionic emulsion based cream with an optimum pH and further evaluated for in vitro drug release characteristics using cellulose membrane, pig skin and human cadaver skin. The hierarchy of drug release was observed to be as follows: HPMC gel system > non-ionic emulsion based cream > anionic emulsion based cream. Further, the effects of various penetration enhancers like Propylene Glycol (PG) , Dimethyl Sulfoxide (DMSO) and Diethylene glycol modoethyl ether (DGME) at a concentration of 5%, 10% and 15% on drug release were evaluated. In most cases, the addition of enhancers had a little or no effect in enhancing the drug release from these bases.;Furthermore, Pig skin and Human cadaver skin were used as a barrier to assess the in-vivo drug release from the formulation. The release of drug was significantly reduced compared to cellulose membrane data with the similar release pattern. The release data were treated to determine the physical parameters that influence drug diffusion, and the values for the steady flux and diffusion coefficient were found to be the highest with HPMC gel based formulation containing 1% Indomethacin with 5 % DMSO as the penetration enhancer yielding the lowest values for the lag time and partition coefficient.
机译：消炎痛/吲哚美辛是一种非甾体抗炎药（NSAID），具有退烧和镇痛作用。消炎痛已被证明是一种有效的消炎药，适合长期用于类风湿性关节炎，强直性脊柱炎和骨关节炎。吲哚美辛可以三种不同的强度制成胶囊剂型25； 50和SR 75毫克。它也可以悬浮液形式以25 mg / ml和50 mg栓剂的浓度提供。口服非选择性COX抑制剂NSAIDs的主要缺点是它们可能对肾脏有毒并增加胃肠道出血的风险。使用NSAID的人群罹患严重胃肠道（GI）并发症的风险增加。消炎痛，美洛昔康，布洛芬等非甾体类抗炎药可能会引起溃疡，出血或胃或肠的孔洞。服用非甾体类抗炎药（NSAIDs）的人患心脏病或中风的风险也增加了。试图评估开发这种药物局部用药的可行性，以此来克服当以口服剂型给药时会引起胃肠道并发症和心血管疾病风险纤维素膜，猪皮和人体尸体皮。观察到药物释放的层次如下：HPMC凝胶系统>非离子乳液基乳膏>阴离子乳液基乳膏。此外，评估了浓度为5％，10％和15％的各种渗透促进剂，如丙二醇（PG），二甲基亚砜（DMSO）和二甘醇二甲基醚（DGME）对药物释放的影响。在大多数情况下，添加增强剂对增强药物从这些碱中的释放几乎没有作用。此外，猪皮和人体尸体皮肤被用作评估制剂中体内药物释放的障碍。与具有类似释放模式的纤维素膜数据相比，药物的释放显着减少。处理释放数据以确定影响药物扩散的物理参数，并且在含有1％吲哚美辛和5％DMSO作为渗透增强剂的HPMC凝胶基制剂中，稳定通量和扩散系数的值最高。滞后时间和分配系数的最小值。

著录项

  • 作者

    Yadav, Neha.;

  • 作者单位

    Long Island University, The Brooklyn Center.;

  • 授予单位 Long Island University, The Brooklyn Center.;
  • 学科 Health Sciences Pharmacy.
  • 学位 M.S.
  • 年度 2014
  • 页码 166 p.
  • 总页数 166
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

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